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structure-based design

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15

Inhibitors & Agonists

1

Biochemical Assay Reagents

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-126247
    BI-2852

    		Ras Cancer
    BI-2852 is a KRAS inhibitor for the switch I/II pocket (SI/II-pocket) by structure-based agent design with nanomolar affinity. BI-2852 is mechanistically distinct from covalent KRASG12C inhibitor (binds to switch II pocket) and binds ten-fold more strongly to active KRASG12D versus KRASwt (740 nM vs 7.5 μM). BI-2852 blocks GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in KRAS mutant cells.
    BI-2852
  • HY-126247B
    (R)-BI-2852

    		Drug Derivative Ras Cancer
    (R)-BI-2852 is the isomer of BI-2852 (HY-126247), and can be used as an experimental control. BI-2852 is a KRAS inhibitor for the switch I/II pocket (SI/II-pocket) by structure-based agent design with nanomolar affinity. BI-2852 is mechanistically distinct from covalent KRASG12C inhibitor (binds to switch II pocket) and binds ten-fold more strongly to active KRASG12D versus KRASwt (740 nM vs 7.5 μM). BI-2852 blocks GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in KRAS mutant cells.
    (R)-BI-2852
  • HY-178297
    VHR-IN-7

    		Phosphatase Cancer
    VHR-IN-7 is a selective vaccinia H1-related (VHR) phosphatase inhibitor with an IC50 of 71 nM. VHR-IN-7 shows very weaker inhibitory activity against MKP-1 (IC50 = 0.47 μM), CD45 (IC50 = 0.3 μM), Cdc25A (IC50 = 3.4 μM), PTP1B (IC50 = 0.59 μM), and HePTP (IC50 = 1.2 μM). VHR-IN-7 inhibits the proliferation of HeLa cells. VHR-IN-7 can be used for the research of cervical cancer .
    VHR-IN-7
  • HY-178292
    VHR-IN-3

    		Phosphatase Cancer
    VHR-IN-3 (Compound 1) is a selective vaccinia H1-related (VHR) phosphatase inhibitor with a Ki of 0.81 μM. VHR-IN-3 mimics the phosphate group through the sulfonic acid group and competitively binds to the catalytic active center of VHR. VHR-IN-3 can be used for the research of cervical cancer .
    VHR-IN-3
  • HY-178296
    VHR-IN-6

    		Phosphatase Cancer
    VHR-IN-6 is a selective vaccinia H1-related (VHR) phosphatase inhibitor with an IC50 of 74 nM. VHR-IN-6 shows very weaker inhibitory activity against MKP-1 (IC50 = 0.52 μM), CD45 (IC50 = 0.50 μM), Cdc25A (IC50 = 2.8 μM), PTP1B (IC50 = 0.42 μM), and HePTP (IC50 = 0.87 μM). VHR-IN-6 inhibits the proliferation of HeLa cells. VHR-IN-6 can be used for the research of cervical cancer .
    VHR-IN-6
  • HY-178285
    VHR-IN-2

    		Phosphatase Cancer
    VHR-IN-2 (Compound SA9) is a selective vaccinia H1-related (VHR) phosphatase inhibitor with an IC50 of 3.1 μM. VHR-IN-2 can be used for the research of cervical cancer .
    VHR-IN-2
  • HY-178301
    VHR-IN-9

    		Phosphatase Cancer
    VHR-IN-9 is a selective vaccinia H1-related (VHR) phosphatase inhibitor with an IC50 of 270 nM. VHR-IN-9 shows very weaker inhibitory activity against MKP-1 (IC50 = 2.8 μM), CD45 (IC50 = 1.8 μM), Cdc25A (IC50 = > 10 μM), PTP1B (IC50 = 2.2 μM), and HePTP (IC50 = 2.4 μM). VHR-IN-9 inhibits the proliferation of HeLa cells. VHR-IN-9 can be used for the research of cervical cancer .
    VHR-IN-9
  • HY-178295
    VHR-IN-5

    		Phosphatase Cancer
    VHR-IN-5 is a selective vaccinia H1-related (VHR) phosphatase inhibitor with an IC50 of 78 nM. VHR-IN-5 shows very weaker inhibitory activity against MKP-1 (IC50 = 0.78 μM), CD45 (IC50 = 0.61 μM), Cdc25A (IC50 = 3.4 μM), PTP1B (IC50 = 1.8 μM), and HePTP (IC50 = 1.5 μM). VHR-IN-5 inhibits the proliferation of HeLa cells. VHR-IN-5 can be used for the research of cervical cancer .
    VHR-IN-5
  • HY-178303
    VHR-IN-8

    		Phosphatase Cancer
    VHR-IN-8 (Compound SA8) is a selective vaccinia H1-related (VHR) phosphatase inhibitor with an IC50 of 2.4 μM. VHR-IN-8 can be used for the research of cervical cancer .
    VHR-IN-8
  • HY-178760
    TGF-8027

    		5-HT Receptor Neurological Disease
    TGF-8027 is a selective 5-HT2A agonist that can cross the blood-brain barrier. TGF-8027 exhibits EC50s of 3.3 nM, 160 nM and 7600 nM against 5-HT2A, 5-HT2C and 5-HT2B and exhibits EC50s against mouse 5-HT2A and mouse 5-HT2C of 14 and 210 nM. TGF-8027 can induce a head-shaking response in mice. TGF-8027 can be used to study diseases that target the 5-HT2A receptor (such as depression) .
    TGF-8027
  • HY-153264
    TAS2R14 agonist-1

    		Taste Receptor Others
    TAS2R14 agonist is a potent TAS2R14 partial agonist with an EC50 of 116.6 ±23.6 nM .
    TAS2R14 agonist-1
  • HY-I0314
    1H-Pyrazole-4-boronic acid pinacol ester

    		Drug Intermediate Others
    1H-Pyrazole-4-boronic acid pinacol ester is a drug intermediate that can be used for the synthesis of Mps1 kinase inhibitors .
    1H-Pyrazole-4-boronic acid pinacol ester
  • HY-120281
    ST-168

    		MEK PI3K Akt Apoptosis Caspase Cancer
    ST-168 is an orally active MEK/PI3K inhibitor with an IC50 of 182 nM against MEK1 and IC50 values ​​of 69.2, 41.7, 1482 and 2293 nM against PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ respectively. ST-168 completely inhibits the phosphorylation of ERK1/2 and AKT and induces cancer cell death in a 3D tumor sphere model. ST-168 demonstrates significant antitumor effects in the A375 melanoma mouse model. ST-168 improves the ocular toxicity profile of MEK inhibitors, showing lower caspase activation levels, indicating reduced apoptosis induction. ST-168 can be used in melanoma research .
    ST-168
  • HY-136742
    BACE2-IN-1

    		Beta-secretase Metabolic Disease
    BACE2-IN-1 (compound 3l) is a highly selective BACE2 inhibitor with a K i value of 1.6 nM. BACE2 inhibitors can be used to research of Type 2 Diabetes .
    BACE2-IN-1
  • HY-W800162
    VEGFR-2-IN-37

    		VEGFR Cancer
    VEGFR-2-IN-37 (compound 12) is an inhibitor of VEGFR-2. The inhibition rate at 200 μM was approximately 56.9 μM. VEGFR-2-IN-37 is a potential inhibitor of human umbilical vein endothelial cell (HUVEC) proliferation .
    VEGFR-2-IN-37

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